GSK963-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK963Cat.No.:HY-103028ACASNo.:2049868-46-2分⼦式:C₁₄H₁₈N₂O分⼦量:230.31作⽤靶点:RIPkinase作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(108.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.3420mL21.7099mL43.4197mL5mM0.8684mL4.3420mL8.6839mL10mM0.4342mL2.1710mL4.3420mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(10.85mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(10.85mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GSK963⼀种⼿性的、强效的、选择性的受体相互作⽤蛋⽩1(RIP1)酶的抑制剂，其IC50值为29nM。GSK963对体外⼩⿏和⼈细胞的坏死具有强效和选择性的抑制作⽤。IC50&TargetIC50:29nM(RIP1inFPbindingassay)[1].体外研究GSK963is>10ꢀ000-foldselectiveforRIP1over339otherkinases,lacksmeasurableactivityagainstIDOandhasaninactiveenantiomer,GSK962,whichcanbeusedtoconfirmon-targeteffects[1].体内研究GSK963(2mg/kg)resultsinacompleteprotectionfromTNF+zVAD-inducedtemperatureloss.GSK963(0.2ꢀmg/kg)alsoshowsasignificantresponse[1].AnimalModel:C57BL/6mice[1].Dosage:0.2mg/kg,2mg/kg,10ꢀmg/kg.Administration:IPonce.Result:ProtectedmicefromTNF+zVAD-inducedhypothermia.REFERENCES[1].BergerSB,etal.CharacterizationofGSK'963:astructurallydistinct,potentandselectiveinhibitorofRIP1kinase.CellDeathDiscov.2015Jul27;1:15009.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8